EDTA体内络合减低^(223)Ra胃肠道辐射损伤的初步实验动物研究  

Preliminary experimental animal study on reducing ^(223)Ra gastrointestinal radiation injury by EDTA complexation in vivo

作　　者：李丹妮 李潇 杨剑[1] 贾国荣[1] 彭烨[1] 左长京[1] LI Danni;LI Xiao;YANG Jian;JIA Guorong;PENG Ye;ZUO Changjing(Department of Nuclear Medicine,Shanghai Changhai Hospital,Shanghai 200433,China)

机构地区：[1]上海长海医院核医学科,上海200433

出　　处：《核技术》2022年第4期39-43,共5页Nuclear Techniques

基　　金：上海市"医苑新星"青年医学人才培养资助计划(沪卫人事[2020]087号);海军军医大学(第二军医大学)长海医院"234学科建设攀峰计划"项目(No.2019YPT002、No.2020YPT002);上海市卫生健康委员会先进适宜技术推广项目(No.2019SY029)资助。

摘　　要：^(223)RaCl_(2)作为针对肿瘤骨转移的α内照射药物,在肿瘤骨转移病灶沉积的同时会有较大比例的肠道富集,引起一定的毒副作用。本研究利用对Ra;离子具有络合作用的乙二胺四乙酸(Ethylenediaminetetraacetic Acid,EDTA)进行体内结合的方式,促进胃肠道沉积的;Ra排出体外。相较于EDTA灌胃导致的;Ra在胃肠道二次富集,经静脉注射的EDTA更有助于;Ra的胃肠道清除。在;^(223)RaCl_(2)给药后2 h经尾静脉按1 mg·kg;注射EDTA后,肠道在6 h的;Ra清除率由(21.3±5.6)%提高到(46.9±4.4)%,同时骨特异性摄取未受明显影响。上述结果提示:静脉注射EDTA络合的方式有助于降低;^(223)RaCl_(2)给药后的胃肠道辐射损伤。[Background];Ra dichloride(^(223)RaCl_(2)) is an α internal irradiation drug for the treatment of bone metastases. In addition to deposition in bone metastatic lesions,223Ra is mostly enriched in the intestines, causing toxic and side effects. [Purpose] This study aims to propose a strategy for promoting excretion of223Ra deposited in the gastrointestinal tract to exploit ethylenediaminetetraacetic acid(EDTA) as a complexing agent for binding of Ra2+ions in vivo. [Methods] Firstly, the in vivo distribution of^(223)RaCl_(2)in rats was evaluated by SPECT/CT at different time points. Then the intravenous and gavage administration were compared side-by-side to determine whether the route of EDTA administration affected the capacity of promoting the excretion of223Ra. At last, the effects of EDTA intervention on bone uptake and the protective effect on the gut were assessed by SPECT/CT imaging and quantitative analysis of radioactive counts. [Results] The total counts of radioactive uptake in rat bone reach 86.3%of the peak at 2 h after^(223)RaCl_(2)injection, and reach the peak(1 405±21) at 12 h after injection. The intestinal clearance of223Ra is increased from(21.3±5.6)% to(46.9±4.4)% at 6 h after EDTA intravenous dose of 1 mg·kg;behind the EDTA administration at 2 h after^(223)RaCl_(2)injection, meanwhile, the bone-specific deposition is unaffected.[Conclusions] The in vivo complexation of intravenous EDTA administration appears to reduce the gastrointestinal radiation injury after^(223)RaCl_(2)injection.

关 键 词：^(223)RaCl_(2) EDTA 骨转移 胃肠道 体内络合 

分 类 号：TL99[核科学技术—核技术及应用]